Pharmaceutical preparation for controlling water-soluble drug release

Abstract

A solid formulation comprising a water-soluble drug and a hardly water-soluble pharmaceutically-acceptable solid substance, which comprises silicone as a carrier, wherein the silicone formulation can exhibit an excellent controlled-release of the water-soluble drug.

1 . A parenteral solid formulation comprising a water-soluble drug and a hardly water-soluble pharmaceutically-acceptable solid substance, which comprises silicone as a carrier. 
     
     
         2 . The parenteral solid formulation of  claim 1  wherein the hardly water-soluble substance is low substituted hydroxypropylcellulose, partly pregelatinized starch, crospovidone, croscarmellose sodium, myristic acid, cholesterol and/or saccharin. 
     
     
         3 . The parenteral solid formulation of  claim 1  wherein the hardly water-soluble substance is low substituted hydroxypropylcellulose and/or cholesterol. 
     
     
         4 . The parenteral solid formulation of  claim 1  wherein the hardly water-soluble substance is contained in 3 to 35% by weight per the whole weight of the formulation. 
     
     
         5 . The parenteral solid formulation of  claim 1  wherein the silicone is contained in 55% or more by weight per the whole weight of the formulation. 
     
     
         6 . The parenteral solid formulation of  claim 1  further comprising a water-soluble additive agent. 
     
     
         7 . The parenteral solid formulation of  claim 6  wherein the water-soluble additive agent is sodium chloride, glucose, mannitol, lactose, glycine, sodium cholate, sodium desoxycholate and/or sodium glycocholate. 
     
     
         8 . The parenteral solid formulation of  claim 6  wherein the water-soluble additive agent is sodium chloride and/or sodium desoxycholate. 
     
     
         9 . The parenteral solid formulation of  claim 8  wherein the hardly water-soluble substance is low substituted hydroxypropylcellulose, and the water-soluble additive agent is sodium chloride. 
     
     
         10 . The parenteral solid formulation of  claim 8  wherein the hardly water-soluble substance is cholesterol, and the water-soluble additive agent is sodium chloride and sodium desoxycholate. 
     
     
         11 . The parenteral solid formulation of  claim 1  wherein the total weight of the water-soluble drug, the hardly water-soluble substance and the optional water-soluble additive agent is 10 to 40% per the whole weight of the formulation, provided that the total weight of the water-soluble drug and the water-soluble additive agent is not more than 35% per the whole weight of the formulation. 
     
     
         12 . The parenteral solid formulation of  claim 1  comprising essentially a water-soluble drug, a pharmaceutically acceptable hardly water-soluble solid substance, and an optional water-soluble additive agent, and which comprises silicone as a carrier. 
     
     
         13 . The parenteral solid formulation of  claim 1  which is a matrix formulation. 
     
     
         14 . The parenteral solid formulation of  claim 1  which is an implantable formulation.